The invention relates to leaves of Cajanus Cajan(L.)Millsp. and extract ,and pharmaceutical formulations thereof. The invention also relate to new uses of leaves of Cajanus Cajan(L.)Millsp. and extract, especially in pharmaceutical filed. The invention belongs to field of Chinese Traditional Medicine.
Cajanus Cajan(L.)Millsp. is a subtropical bush plant, which belongs to adjonus genus of popilionaccae family, grows in south part of China, and also is called as Liudou, Niudou, Dourong or Liudian in Chinese. The plant has effects of clearing away heat and detoxicating, promoting blood circulation and relieving blood stasis, antisepsis, relieving inflammatory. Its root has effects of clearing away heat and detoxicating, stopping bleeding and relieving pain, and killing parasites. The tender leaves of it can be used in treating aphtha when chewed in mouth; the juice pressed from its tender leaves can be used in treating jaundice; the pulp obtained by pounding its tender leaves have the function of eliminating slough and promoting tissue regeneration on wound; the decoction of its leaves can be effective in cough and diarrhea. CN 11 74052A disclosed medical use of Cajanus Cajan(L.)Millsp., however, it is not clear to obtain active component of the plant because it was used in combination with other components and wasn""t extracted. Therefor, its use is limited.
It is an object of the invention to provide an extract from leaves of Cajanus Cajan(L.)Millsp., so-called its active component.
It is a further object of this invention to provide a process for the preparation of such extract.
It is also a object of this invention to provide an pharmaceutical formulation comprising leaves of Cajanus Cajan(L.)Millsp. or its extract as active component.
It is another object of this invention to provide new use of leaves of Cajanus Cajan(L.)Millsp. or its extract, that is new use in the preparation of pharmaceutical formulations.
The extract of leaves of Cajanus Cajan(L.)Millsp. can be obtained as follows:
(1) The Purification and Preparation of Crude Materials
Cajanus Cajan(L.)Millsp.
[preparation] :The tender leaves and branches of Cajanus Cajan(L.)Millsp. is collected, removed impurity and old branches, cleaned and dried in the shade. They are cut into about 5 cm small parts and put in clean container for later use.
(2) Extraction, Concentrating and Drying of Drugs
These treated Cajanus Cajan(L.)Millsp. are put in multi-function extractor. Water is added in 10-fold amount of drugs, and then these drugs are immersed for about 0.5 to 2 hours. The mixture is decocted 14 times for 1-2 hours each times. After filtered, the filtrates is drew immediately into a vacuum concentrator(atmospheric pressure is xe2x88x920.08 Mpa and temperature is 60xc2x0 C.) and concentrated to relative density of 1.05-1.15 (detected at 60xc2x0 C.). After filtered with 80 mush filter cloth, the filtrates is filtered by continuous centrifugation, and then the centrifugal fluid is dried by spray-drying process to obtain dried extract powder, that is the active component extract according to the invention which is put in clean and air-tight container.
In order to produce extract according to the invention, the preferable process includes the following steps. These treated Cajanus Cajan(L.)Millsp. are put in multi-function extractor. After water is added in 10-fold amount of drugs and these drugs are immersed for about 1 hour, the mixture is decocted 3 times for 1.5 hours each times. After filtered, the filtrates is drew immediately into a vacuum concentrator and concentrated under the condition of xe2x88x920.08 Mpa and 60xc2x0 C. to relative density of 1.05-1.15 (detected at 60xc2x0 C.). After filtered with 80 mush filter clothes, the filtrates is filtered by continuous centrifugation at 15,000 r.p.m with the flow amount of 50L/hour, and then the centrifugal fluid is dried by spray-drying process under the condition of 180xc2x0 C. at entrance, 4 seconds of dried time and 80xc2x0 C. at exit. The resultant dried extract powder is put in clean and air-tight container.
The extract of leaves of Cajanus Cajan(L.)Millsp. can be formulated into pharmaceutical formulations for clinic use such as tablets, pills, powders, capsules, oral liquids and so on by standard methods, in which the extract is present as active component at effective therapeutic amount, in generally range from 0.01 to 99.9%, preferably, 1 to 90%, more preferably from 5 to 80%, most preferably from 10 to 70%. Alternatively, dried leaves of Cajanus Cajan(L.)Millsp. can be ground to powder as active component to formulated into clinic pharmaceutical formulations by standard methods.
The capsule of leaves of Cajanus Cajan(L.)Millsp. can be produced by mixing the extract optionally with excipient such as starch and filling into capsule. It is confirmed by tests that leaves of Cajanus Cajan(L.)Millsp. or extract thereof have the following novel medical uses.
1. The Use of Leaves of Cajanus Cajan(L.)Millsp. or Extract Thereof for Manufacture of a Medicament for the Treatment of Osteoporosis
In order to observe the effect of the capsule of leaves of Cajanus Cajan(L.)Millsp on experimental osteoporosis, the osteoporosis model is made by tretinoin. The result indicated that the capsule notably increased levels of calcium and phosphorus in serum, decreased the level of alkaline phosphatase, and enhanced BMC and BMD in rats. From the observation on pathological section, it is showed that the capsule significantly improved the quality of bone trabecula, reduced the numbers of osteoclast and promoted the growth of osteoblast and thereby prevented and treated osteoporosis.
2. The Use of Leaves of Cajanus Cajan(L.)Millsp. or Extract Thereof for Manufacture of a Medicament for the Treatment of Ischemic Necrosis of Caput Femoris
After established the New Zealand rabbit model of ischemic necrosis of caput femoris by horse serum-hormone, the capsule at high, middle and low dosages was administrated to the animals separately, normal control group and model control group were set simultaneously. The result showed that the capsule had notable effect on treatment of hormone-induced ischemic necrosis of caput femoris after detecting the density of bone tissue in proximal end of femur, observing by magnifying X-ray photo, pathologic examination by light microscope, observing under television microscope and dynamic measurement for metabolism of bone tissue.
3. The Effect of Leaves of Cajanus Cajan(L.)Millsp. or Extract Thereof on the Improvement of Hemorrheology
The test of microcirculation in rat mesentery demonstrated that the capsule can significantly increase velocity of blood flow, infinitesimal calculus of velocity and state of blood flow. The index of hemorrheology for rat acute hypostasis model displayed that the capsule can enhance the specific viscosity of total blood and plasma and decrease blood sedimentation.
4. The Use of Leaves of Cajanus Cajan(L.)Millsp. or Extract Thereof for Manufacture of a Medicament for Anti-inflammatory and Analagecization
The tests of dimethylbenzene induced inflammation on mice pinna and cotton ball granuloma on mice showed that the capsule can alleviated notably ear tumefaction reduced by dimethylbenzene and cotton ball granuloma. Tests of torsion method and hot plate method on mice showed that the capsule declined clearly the number of torsion mice, prolonged the period of the first torsion, increased percent of analgesis, and increased threshold value of pain on mice.
5. The Use of Leaves of Cajanus Cajan(L.)Millsp. or Extract Thereof for Manufacture of a Medicament for Enhancement of Immune Function
Mice were induced by prednisone acetate to low immune function. In these models, the capsule according to the invention not only have the trend of enhancing phagocytic function of mononuclear leukocyte in mice, but also increased markedly the weight of immune organs such as thymus, spleen and the level of hemolysin in mice in which chicken red blood cell acts as immunogen. In addition, It significantly increased the present rate of transition state T-lymphoblastoid cell and the rate of transformation of lymphocyte stimulated by phytohematoagglutinin in mice.
6. The Use of Leaves of Cajanus Cajan(L.)MilIsp or Extract Thereof for Manufacture of a Medicament for the Treatment of Bed Sore
It can be seen by clinical observation that the curative effect of leaves of Cajanus Cajan(L.)Millsp. and extract thereof are superior to that of traditional ointment for promoting muscle growth on treatment of bed sore. The leaves of Cajanus Cajan(L.)Millsp. and extract thereof can not only shorten course of treatment, but also decrease the scar after healing.
7. The Use of Leaves of Cajanus Cajan(L.)Millsp. or Extract Thereof for Manufacture of a Medicament for the Treatment of Infected Wound
The leaves of Cajanus Cajan(L.)Millsp. and extract thereof have effects of promoting the growth of epithelium granulation tissue on surface of wound, increasing supply of blood to surface of wound, speeding up wound healing, decreasing growth of scar tissue, and enhancing the quality of healing. As far as anti-infectious effect is concerned, it can be found that leaves of Cajanus Cajan(L.)Millsp. and extract thereof have good effect against infection on infected wound, which is manifested by quickly disappear of wound and inflammatory reaction, especially by decreasing rapidly the exudation on surface of wound after administration and clean surface of wound, it is implied that the medication has good effect on resisting inflammatory exudation.
8. The Use of Leaves of Cajanus Cajan(L.)Millsp. or Extract Thereof for Manufacture of a Medicament for the Treatment of Infected Wound of Open Fracture
The leaves of Cajanus Cajan(L.)Millsp. and extract thereof have good effect of anti-infection in clinical test and can promote the growth of granulation tissue, increase the supply blood for wound surface, enhance the healing of wound surface, particularly the growth of granulation tissue, as called xe2x80x9cgranulation island of bonexe2x80x9d, on the bone surface exposed to wound surface.
The results of clinical treatment also showed that the leaves of Cajanus Cajan(L.)Millsp. and extract thereof have good curative effect on angina pectoris of coronary heart disease, cerebral infraction, and fracture.
In order to understand the essence of the invention further, the process of producing the extract of Cajanus Cajan(L.)Millsp., the pharmacological study of leaves of Cajanus Cajan(L.)Millsp. and extract thereof as well as the results of study will be described in detail by means of the following examples so as to illustrate the novel uses in pharmaceutical field.